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In order to deliver several drugs and activities for different objectives, lipid nanocarriers were developed. Still, the in vivo fate of such carriers remains questionable. Although majority of the lipids undergo biotransformation and deemed to be eliminated by common elimination pathways, researchers need to ensure their complete eradication after the drug has been completely released from such carriers. Nonetheless, several obstacles for lipid nanocarriers are still a hot topic for drug therapy among the most interesting and recent assignments for lipid nanocarriers. Cancer treatment, blood-brain barrier (BBB) elimination, and protein and gene delivery are fields of study where a healthy and reliable carrier of drug is essential, and lipid nanocarriers for such purposes are suggested and investigated.